- GAVRETO® (pralsetinib) is an FDA approved
targeted therapy for the treatment of RET fusion-positive
metastatic non-small cell lung cancer and advanced or
metastatic thyroid cancer
- Acquisition of established U.S. marketed product further
expands Rigel's portfolio and leverages Rigel's existing
infrastructure in both the institutional and community
settings
- GAVRETO generated ~$28M in
U.S. net product sales in 2023
SOUTH
SAN FRANCISCO, Calif., Feb. 22,
2024 /PRNewswire/ -- Rigel Pharmaceuticals, Inc.
("Rigel") (Nasdaq: RIGL) today announced that it has entered into a
definitive agreement to acquire the U.S. rights to
GAVRETO® (pralsetinib) from Blueprint Medicines
Corporation ("Blueprint"). GAVRETO is a once daily, small molecule,
oral, kinase inhibitor of wild-type RET (rearranged during
transfection) and oncogenic RET fusions. GAVRETO is approved by the
U.S. Food and Drug Administration (FDA) for the treatment of adult
patients with metastatic RET fusion-positive non-small cell lung
cancer (NSCLC) as detected by an FDA approved test.
"NSCLC is the most common type of lung cancer in the U.S. with
RET fusions representing 1-2% of the patient population. GAVRETO is
a targeted treatment option with an established safety profile that
has shown durable responses in RET fusion-positive NSCLC
patients and represents a compelling addition to our commercial
portfolio," said Raul Rodriguez,
Rigel's president and CEO. "We are excited about this transaction,
as we continue to realize our corporate strategy to grow our
hematology and oncology business while leveraging our existing
commercial and medical affairs infrastructure and expertise.
GAVRETO is the third commercial product in our portfolio,
supporting top line growth and our commitment to providing
differentiated therapies to patients in need."
"GAVRETO is one of only two approved RET inhibitors on the
market for patients. We are confident in our ability to effectively
transition GAVRETO to our distribution network and utilize our
robust capabilities to enable both existing and new patients to
continue to have access to this important treatment option," said
Dave Santos, Rigel's chief
commercial officer. "The addition of GAVRETO will be highly
synergistic with our current product portfolio, leveraging our
existing commercial infrastructure and enabling us to expand into
solid tumors."
GAVRETO is also approved for the treatment of adult and
pediatric patients 12 years of age and older with advanced or
metastatic RET fusion-positive thyroid cancer who require systemic
therapy and who are radioactive iodine-refractory (if radioactive
iodine is appropriate). This indication was approved under
accelerated approval based on overall response rate and duration of
response. Continued approval for this indication may be contingent
upon verification and description of clinical benefit in
confirmatory trial(s). Discussions with the FDA regarding
confirmatory requirements are ongoing.
Under the terms of the agreement, Blueprint will receive a
purchase price of $15.0 million,
$10.0 million of which is payable
upon first commercial sale by Rigel and an additional $5.0 million of which is payable on the first
anniversary of the closing date, subject to certain conditions.
Blueprint is also eligible to receive up to $97.5 million in future commercial milestone
payments and up to $5.0 million in
future regulatory milestone payments, in addition to tiered
royalties ranging from 10% to 30%. Patents that have issued or are
expected to issue covering GAVRETO will have statutory expiration
dates between 2036 and 2041. Rigel expects to complete the
transition of the asset and start recognizing product sales in the
third quarter of 2024. Rigel will provide additional details on
this transaction at its upcoming quarterly earnings call in early
March.
Rigel's acquisition of the U.S. rights to GAVRETO is concurrent
to a previously announced Roche decision to terminate the GAVRETO
collaboration agreement with Blueprint effective February 22, 2024. According to a statement from
the company, Genentech, a member of the Roche Group, is committed
to patients and working with Rigel and Blueprint to ensure current
and newly prescribed patients can access GAVRETO without
interruption through the transition period, with specific next
steps and timing to be communicated to key stakeholders, including
healthcare providers, in the next few weeks.
About NSCLC
It is estimated that over 230,000 adults
in the U.S. will be diagnosed with lung cancer in 2024. Lung
cancer is the leading cause of cancer death in the U.S, with NSCLC
being the most common type accounting for 80-85% of all lung cancer
diagnoses.1 RET fusions are implicated in
approximately 1-2% of patients with NSCLC.2
About GAVRETO® (pralsetinib)
INDICATIONS
GAVRETO (pralsetinib) is indicated for the treatment
of:
- Adult patients with metastatic rearranged during transfection
(RET) fusion-positive non-small cell lung cancer (NSCLC) as
detected by an FDA-approved test
- Adult and pediatric patients 12 years of age and older with
advanced or metastatic RET fusion-positive thyroid cancer who
require systemic therapy and who are radioactive iodine-refractory
(if radioactive iodine is appropriate)*
*This indication is approved under accelerated approval based on
overall response rate and duration of response. Continued approval
for this indication may be contingent upon verification and
description of clinical benefit in confirmatory trial(s).
IMPORTANT SAFETY INFORMATION
- Interstitial Lung Disease (ILD)/Pneumonitis: Severe,
life-threatening, and fatal ILD/pneumonitis can occur in patients
treated with GAVRETO. Pneumonitis occurred in 12% of patients who
received GAVRETO, including 3.3% with Grade 3-4, and 0.2% with
fatal reactions. Monitor for pulmonary symptoms indicative of
ILD/pneumonitis. Withhold GAVRETO and promptly investigate for ILD
in any patient who presents with acute or worsening of respiratory
symptoms (e.g., dyspnea, cough, and fever). Withhold, reduce dose
or permanently discontinue GAVRETO based on severity of confirmed
ILD.
- Hypertension: Occurred in 35% of patients, including
Grade 3 hypertension in 18% of patients. Overall, 8% had their dose
interrupted and 4.8% had their dose reduced for hypertension.
Treatment-emergent hypertension was most commonly managed with
anti-hypertension medications. Do not initiate GAVRETO in patients
with uncontrolled hypertension. Optimize blood pressure prior to
initiating GAVRETO. Monitor blood pressure after 1 week, at least
monthly thereafter and as clinically indicated. Initiate or adjust
anti-hypertensive therapy as appropriate. Withhold, reduce dose, or
permanently discontinue GAVRETO based on the severity.
- Hepatotoxicity: Serious hepatic adverse reactions
occurred in 1.5% of patients treated with GAVRETO. Increased
aspartate aminotransferase (AST) occurred in 49% of patients,
including Grade 3 or 4 in 7% and increased alanine aminotransferase
(ALT) occurred in 37% of patients, including Grade 3 or 4 in 4.8%.
The median time to first onset for increased AST was 15 days
(range: 5 days to 2.5 years) and increased ALT was 24 days (range:
7 days to 3.7 years). Monitor AST and ALT prior to initiating
GAVRETO, every 2 weeks during the first 3 months, then monthly
thereafter and as clinically indicated. Withhold, reduce dose or
permanently discontinue GAVRETO based on severity.
- Hemorrhagic Events: Serious, including fatal,
hemorrhagic events can occur with GAVRETO. Grade ≥3 events occurred
in 4.1% of patients treated with GAVRETO including one patient with
a fatal hemorrhagic event. Permanently discontinue GAVRETO in
patients with severe or life-threatening hemorrhage.
- Tumor Lysis Syndrome (TLS): Cases of TLS have been
reported in patients with medullary thyroid carcinoma receiving
GAVRETO. Patients may be at risk of TLS if they have rapidly
growing tumors, a high tumor burden, renal dysfunction, or
dehydration. Closely monitor patients at risk, consider appropriate
prophylaxis including hydration, and treat as clinically
indicated.
- Risk of Impaired Wound Healing: Impaired wound healing
can occur in patients who receive drugs that inhibit the vascular
endothelial growth factor (VEGF) signaling pathway. Therefore,
GAVRETO has the potential to adversely affect wound healing.
Withhold GAVRETO for at least 5 days prior to elective surgery. Do
not administer for at least 2 weeks following major surgery and
until adequate wound healing. The safety of resumption of GAVRETO
after resolution of wound healing complications has not been
established.
- Embryo-Fetal Toxicity: Based on findings from animal
studies and its mechanism of action, GAVRETO can cause fetal harm
when administered to a pregnant woman. Advise pregnant women of the
potential risk to a fetus. Advise females of reproductive potential
to use effective non-hormonal contraception during treatment with
GAVRETO and for 2 weeks after the last dose. Advise males with
female partners of reproductive potential to use effective
contraception during treatment with GAVRETO and for 1 week after
the last dose.
- Common adverse reactions (≥25%) were musculoskeletal
pain, constipation, hypertension, diarrhea, fatigue, edema,
pyrexia, and cough. Common Grade 3/4 laboratory abnormalities
(≥2%) were decreased lymphocytes, decreased neutrophils,
decreased hemoglobin, decreased phosphate, decreased leukocytes,
decreased sodium, increased aspartate aminotransferase (AST),
increased alanine aminotransferase (ALT), decreased calcium
(corrected), decreased platelets, increased alkaline phosphatase,
increased potassium, decreased potassium, and increased
bilirubin.
- Avoid coadministration of GAVRETO with strong or moderate
CYP3A inhibitors, P-gp inhibitors, or combined P-gp and strong or
moderate CYP3A inhibitors. If coadministration cannot be
avoided, reduce the GAVRETO dose. Avoid coadministration of GAVRETO
with strong or moderate CYP3A inducers. If coadministration
cannot be avoided, increase the GAVRETO dose.
- Lactation: Advise women not to breastfeed during
treatment with GAVRETO and for 1 week after the last dose.
- Pediatric Use: Monitor open growth plates in adolescent
patients. Consider interrupting or discontinuing GAVRETO if
abnormalities occur.
You may report side effects to the FDA
at 1-800-FDA-1088 or www.fda.gov/medwatch.
You may also report side effects to Genentech
at 1-888-835-2555.
Please click here to see the full
Prescribing Information and Patient Information for
GAVRETO.
About Rigel
Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL)
is a biotechnology company dedicated to discovering, developing and
providing novel therapies that significantly improve the lives of
patients with hematologic disorders and cancer. Founded in 1996,
Rigel is based in South San Francisco,
California. For more information on Rigel, the Company's
marketed products and pipeline of potential products, visit
www.rigel.com.
- The American Cancer Society. Key Statistics for Lung Cancer.
Revised November 20, 2023. Accessed
February 7,
2024: https://www.cancer.org/cancer/types/lung-cancer/about/key-statistics.html
- Kato, S. et al. RET aberrations in diverse cancers:
next-generation sequencing of 4,871 patients. Clin Cancer Res. 2017 April 15;23(8):1988-1997.
doi: 10.1158/1078-0432.CCR-16-1679
Forward Looking Statements
This press release
contains forward-looking statements relating to, among other
things, the potential benefits of Rigel's acquisition of U.S.
rights to GAVRETO, including opportunities in NSCLC and DTC,
Rigel's ability to leverage its existing commercial infrastructure
to market and distribute GAVRETO, Rigel's ability to transition
GAVRETO to its distribution network and provide patients with
access to GAVRETO, the payment and timing of milestone and royalty
payments and Rigel's ability to start recognizing product sales in
the third quarter of 2024 and the market opportunity for GAVRETO.
Any statements contained in this press release that are not
statements of historical fact may be deemed to be forward-looking
statements. Forward-looking statements can be identified by words
such as "plan", "potential", "may", "expects", "will" and similar
expressions in reference to future periods. Forward-looking
statements are neither historical facts nor assurances of future
performance. Instead, they are based on Rigel's current beliefs,
expectations, and assumptions and hence they inherently involve
significant risks, uncertainties and changes in circumstances that
are difficult to predict and many of which are outside of our
control. Therefore, you should not rely on any of these
forward-looking statements. Actual results and the timing of events
could differ materially from those anticipated in such forward
looking statements as a result of these risks and uncertainties,
which include, without limitation, risks and uncertainties
associated with the commercialization and marketing of GAVRETO;
risks that the FDA or other regulatory authorities may make adverse
decisions regarding GAVRETO; risks that GAVRETO may have unintended
side effects, adverse reactions or incidents of misuses; the
availability of resources to develop market and distribute GAVRETO;
risks related to the transition of GAVRETO to Rigel, including
risks related to the effectiveness of transition services and drug
continuity; market competition for GAVRETO; as well as other risks
detailed from time to time in Rigel's reports filed with the
Securities and Exchange Commission, including its Quarterly Report
on Form 10-Q for the quarter ended September
30, 2023 and subsequent filings. Any forward-looking
statement made by us in this press release is based only on
information currently available to us and speaks only as of the
date on which it is made. Rigel does not undertake any obligation
to update forward-looking statements, whether written or oral, that
may be made from time to time, whether as a result of new
information, future developments or otherwise, and expressly
disclaims any obligation or undertaking to release publicly any
updates or revisions to any forward-looking statements contained
herein, except as required by law.
Contact for Investors & Media:
Investors:
Rigel Pharmaceuticals, Inc.
650.624.1232
ir@rigel.com
Media:
David
Rosen
Argot Partners
212.600.1902
david.rosen@argotpartners.com
View original content to download
multimedia:https://www.prnewswire.com/news-releases/rigel-pharmaceuticals-acquires-us-rights-to-gavreto-302068670.html
SOURCE Rigel Pharmaceuticals, Inc.